On demand administration of clomipramine and salts thereof to treat premature ejaculation

Abstract

A method is provided for delaying the onset of ejaculation in an individual. The method involves systemic and on demand administration to an individual of a pharmaceutical formulation containing an amount of an active agent selected from the group consisting of clomipramine and pharmacologically acceptable acid addition salts thereof. Drug delivery may be accomplished via any route designed to provide systemic levels of the active agent effective to delay the onset of ejaculation. Pharmaceutical formulations and dosage forms are provided as well.

Description

TECHNICAL FIELDThis invention relates generally to methods and pharmaceutical compositions for treating sexual dysfunction; more particularly, the invention relates to treatment of premature ejaculation, preferably by on demand administration of clomipramine or a pharmacologically acceptable acid addition salt thereof.BACKGROUNDPremature ejaculation is a debilitating sexual dysfunction. This dysfunction can lead to an inability to enter or sustain relationships and can cause psychological damage to sufferers. Premature ejaculation can also impair reproductive success.Previous methods of treating premature ejaculation included psychological therapies, topical anesthetics and the use of devices (U.S. Pat. Nos. 5,535,758, 5,063,915, 5,327,910, and 5,468,212). All of these methods have significant drawbacks. Psychological therapies benefit only a subset of patients and require specialized therapists who may not be available to all patients, particularly in remote areas. Furthermore, psy...

AI Technical Summary

Benefits of technology

Accordingly, it is a primary object of the invention to address the above-described need in the art by providing a novel method for delaying the onset of ejaculation by systemically administering on demand a pharmaceutical formulation containing an amount of an active agent selected from the group consisting of clomipramine and pharmacologically acceptable acid addition salts thereof effective to delay the onset of ejaculation by the individual during sexual activity.

It is another object of the invention to provide a dosage form for delaying the onset of ejaculation in a male individual, comprising a rapid-release formulation for systemic absorption containing an amount of an active agent selected from the group consisting of clomipramine and pharmacologically acceptable acid addition salts thereof effective to delay the onset of ejaculation by the individual during sexual activity.

Problems solved by technology

This dysfunction can lead to an inability to enter or sustain relationships and can cause psychological damage to sufferers.

Premature ejaculation can also impair reproductive success.

All of these methods have significant drawbacks.

Psychological therapies benefit only a subset of patients and require specialized therapists who may not be available to all patients, particularly in remote areas.

Furthermore, psychological therapies cannot alleviate premature ejaculation resulting from non-psychological causes.

Anesthetic agents decrease sensitivity of tissues, thereby diminishing sexual pleasure.

Also, topical anesthetics can be transferred to sexual partners and thereby decrease their sensitivity and pleasure as well.

With regard to devices, these can be awkward, inconvenient and embarrassing to use.

Additionally, devices can cause irritation to one or both partners.

However, these drugs may not be effective for all patients, and the side effects of these drugs can halt treatment or impair patient compliance.

Disease states or adverse interactions with other drugs may contraindicate the use of these compounds or require lower dosages that may not be effective to delay the onset of ejaculation.

In addition, many drugs must be administered chronically or at times that are inconvenient.

However, the administration of fluoxetine has many undesired aspects.

U.S. Pat. No. 5,151,448 describes administration of fluoxetine on a daily basis which, according to many clinicians, presents a compliance issue as patients often miss or forget to take their dose.

In addition, patients with hepatic or renal impairments may not be able to use fluoxetine due to its metabolism in the liver and excretion via the kidney.

Systemic events during oral fluoxetine treatment involving the lungs, kidneys or liver have occurred, and death has occurred from overdoses.

In addition, side effects of oral fluoxetine administration include hair loss, nausea, vomiting, dyspepsia, diarrhea, anorexia, anxiety, nervousness, insomnia, drowsiness, fatigue, headache, tremor, dizziness, convulsions, sweating, pruritis and skin rashes.

Individuals taking monoamine oxidase inhibitors cannot take sertraline due to the risk of toxicity, leading to memory changes, confusion, irritability, chills, pyrexia and muscle rigidity.

Like sertraline, paroxetine cannot be given to patients undergoing treatment with a monoamine oxidase inhibitor.

A common side effect of these drugs is postural hypotension.

In addition, daily administration increases the possibility of patients suffering from a drug.times.s undesirable side effects as a result of continuous exposure to the agent.

Such a dosing regimen, however, still fails to provide for a flexible and convenient method for treating premature ejaculation.

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